Mibefradil alters intracellular calcium concentration by activation of phospholipase C and IP₃ receptor function.

ABSTRACT: Mibefradil is a tetralol derivative originally developed as an antagonist of T-type voltage-gated calcium (Ca²⁺) channels to treat hypertension when used at nanomolar dosage. More recently, its therapeutic application in hypertension has declined and has been instead repurposed as a treatment of cancer cell proliferation and solid tumor growth. Beyond its function as a Ca_v blocker, the micromolar concentration of mibefradil can stimulate a rise in [Ca²⁺]_cyt although the mechanism is poorly known. The chanzyme TRPM7 (transient receptor potential melastanin 7), the release of intracellular Ca²⁺ pools, and Ca²⁺ influx by ORAI channels have been associated with the increase in [Ca²⁺]_cyt triggered by mibefra

SUBMITTER: Souza Bomfim GH 

PROVIDER: S-EPMC8607413 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature